In recent years, a tendency has emerged among people, especially young people, to increase the effect of alcohol and/or specific drug substances by intake of for example pain relievers or fever reducers in combination with alcohol. Many pharmaceutical compositions for oral use release the drug substance with a faster release rate in the presence of alcohol and, accordingly, the drug substance is available for absorption at a faster rate than intended by the manufacturer. Such a faster release rate may lead to unwanted and potentially dangerous effects. This may lead to unwanted effects similar to the effect denoted “dose dumping”.
Unintended, rapid drug release in a short period of time of the entire amount or a significant fraction of the drug substance retained in a controlled release dosage form is often referred to as “dose dumping”. It has been reported that some modified-release oral dosage forms contain drug substances and excipients that exhibit higher solubility in ethanolic solutions compared to aqueous media. Such products can be expected to exhibit a more rapid drug dissolution and release rate in the presence of ethanol. Therefore, in theory, concomitant consumption of alcoholic beverages along with these products might be expected to have the potential to induce dose dumping (FDA's ACPS Meeting 2005). However, the problem is not only of relevance for controlled release dosage form, but also for conventional oral dosage forms and for immediate release dosage forms.
Moreover, in the 1990s, Food and Drug Administrations in USA (FDA) announced that for example over-the-counter (OTC) pain relievers and fever reducers must carry a warning label advising consumers who consume three or more alcoholic drinks every day to consult a physician before using these drugs. FDA issued this final rule after considering public comments and data on the effect of combining chronic alcohol ingestion and the use of various OTC analgesics. The action also followed the recommendations of the Nonprescription Drugs Advisory Committee and the Arthritis Drugs Advisory Committee which concluded that chronic alcohol users should be warned that they may be at an increased risk of liver damage or stomach bleeding from use of these drugs. Relevant drug substances are for example aspirin, other salicylates, acetaminophen, ibuprofen, naproxen sodium, or ketoprofen.
A number of controlled release pharmaceutical compositions have been developed that are said to be resistant towards abuse by intake of alcohol. However, there is still a need for developing pharmaceutical compositions with immediate release of a drug substance (analgesics, antipyretics etc.) that also are resistant to abuse by intake of alcohol.